EP2696683A4 - COMPOSITIONS AND THERAPEUTIC APPLICATIONS OF IKK-MEDIATED KINASE EPSILON AND TANK BINDING KINASE-1 HEMMER - Google Patents

COMPOSITIONS AND THERAPEUTIC APPLICATIONS OF IKK-MEDIATED KINASE EPSILON AND TANK BINDING KINASE-1 HEMMER

Info

Publication number
EP2696683A4
EP2696683A4 EP12771276.8A EP12771276A EP2696683A4 EP 2696683 A4 EP2696683 A4 EP 2696683A4 EP 12771276 A EP12771276 A EP 12771276A EP 2696683 A4 EP2696683 A4 EP 2696683A4
Authority
EP
European Patent Office
Prior art keywords
kinase
tankbinding
ikk
inhibitors
compositions
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP12771276.8A
Other languages
German (de)
English (en)
French (fr)
Other versions
EP2696683A1 (en
Inventor
Ryan C Holcomb
Paul R Sebahar
Kazuyuki Suzuki
Donald A Mcleod
David M Dastrup
Christophe Hoarau
Robert J Halter
Matthew Gregory Bursavich
Mark D Shenderovich
Burt Richards
Paul L Bartel
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Alzheimers Institute of America Inc
Original Assignee
Alzheimers Institute of America Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Alzheimers Institute of America Inc filed Critical Alzheimers Institute of America Inc
Publication of EP2696683A1 publication Critical patent/EP2696683A1/en
Publication of EP2696683A4 publication Critical patent/EP2696683A4/en
Withdrawn legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
EP12771276.8A 2011-04-12 2012-04-12 COMPOSITIONS AND THERAPEUTIC APPLICATIONS OF IKK-MEDIATED KINASE EPSILON AND TANK BINDING KINASE-1 HEMMER Withdrawn EP2696683A4 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161474366P 2011-04-12 2011-04-12
PCT/US2012/033384 WO2012142329A1 (en) 2011-04-12 2012-04-12 Compositions and therapeutic uses of ikk-related kinase epsilon and tankbinding kinase 1 inhibitors

Publications (2)

Publication Number Publication Date
EP2696683A1 EP2696683A1 (en) 2014-02-19
EP2696683A4 true EP2696683A4 (en) 2014-08-13

Family

ID=47009699

Family Applications (1)

Application Number Title Priority Date Filing Date
EP12771276.8A Withdrawn EP2696683A4 (en) 2011-04-12 2012-04-12 COMPOSITIONS AND THERAPEUTIC APPLICATIONS OF IKK-MEDIATED KINASE EPSILON AND TANK BINDING KINASE-1 HEMMER

Country Status (10)

Country Link
US (1) US20140288044A1 (ko)
EP (1) EP2696683A4 (ko)
JP (1) JP2014510794A (ko)
KR (1) KR20140048873A (ko)
CN (1) CN103732067A (ko)
AU (1) AU2012242777A1 (ko)
BR (1) BR112013026202A2 (ko)
CA (1) CA2832919A1 (ko)
MX (1) MX2013011908A (ko)
WO (1) WO2012142329A1 (ko)

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GB201012105D0 (en) 2010-07-19 2010-09-01 Domainex Ltd Novel pyrimidine compounds
DE102011112978A1 (de) * 2011-09-09 2013-03-14 Merck Patent Gmbh Benzonitrilderivate
TW201418243A (zh) 2012-11-15 2014-05-16 Bayer Pharma AG 含有磺醯亞胺基團之ｎ－（吡啶－２－基）嘧啶－４－胺衍生物
GB201303109D0 (en) * 2013-02-21 2013-04-10 Domainex Ltd Novel pyrimidine compounds
CN104297354B (zh) * 2013-07-16 2016-07-06 重庆市康乾医药有限公司 一种高效液相色谱法测定盐酸戊乙奎醚中杂质的检测方法
JP6431914B2 (ja) 2013-12-11 2018-11-28 バイオジェン・エムエイ・インコーポレイテッドＢｉｏｇｅｎ ＭＡ Ｉｎｃ． 腫瘍学、神経学及び免疫学におけるヒト疾患の治療に有用なビアリール化合物
PT3089971T (pt) * 2014-01-01 2020-09-03 Medivation Tech Llc Compostos e métodos de utilização
TW201613916A (en) 2014-06-03 2016-04-16 Gilead Sciences Inc TANK-binding kinase inhibitor compounds
CN104020230B (zh) * 2014-06-20 2015-07-15 成都力思特制药股份有限公司 一种用于检测盐酸戊乙奎醚中副产物的方法
CN104090037B (zh) * 2014-06-20 2015-12-30 成都力思特制药股份有限公司 一种盐酸戊乙奎醚的降解产物的检测方法
EA201790395A1 (ru) 2014-09-26 2017-08-31 Джилид Сайэнс, Инк. Производные аминотриазина, подходящие для применения в качестве соединений-ингибиторов tank-связывающей киназы
ES2720525T3 (es) 2014-10-16 2019-07-22 Bayer Pharma AG Derivados fluorados de benzofuranil-pirimidina que contienen un grupo sulfona
WO2017055196A1 (en) 2015-09-29 2017-04-06 Bayer Pharma Aktiengesellschaft Novel macrocyclic sulfondiimine compounds
JP6888000B2 (ja) 2015-10-08 2021-06-16 バイエル ファーマ アクチエンゲゼルシャフト 新規な修飾された大環状化合物
WO2017060322A2 (en) 2015-10-10 2017-04-13 Bayer Pharma Aktiengesellschaft Ptefb-inhibitor-adc
CU20180059A7 (es) 2015-12-17 2018-10-04 Gilead Sciences Inc Compuestos inhibidores de la quinasa de unión a tank
CN106928216A (zh) * 2015-12-31 2017-07-07 中国科学院上海药物研究所 具有erk激酶抑制活性的化合物、其制备方法和用途
EP3190103A1 (en) * 2016-01-08 2017-07-12 Rijksuniversiteit Groningen Inhibitors of the pd-1/pd-l1 protein/protein interaction
AU2017209935B2 (en) 2016-01-22 2021-04-01 Janssen Pharmaceutica Nv New substituted cyanoindoline derivatives as NIK inhibitors
CA3012031C (en) * 2016-01-22 2024-03-26 Janssen Pharmaceutica Nv 6-membered heteroaromatic substituted cyanoindoline derivatives as nik inhibitors
WO2018002219A1 (en) 2016-06-30 2018-01-04 Janssen Pharmaceutica Nv Cyanoindoline derivatives as nik inhibitors
WO2018002217A1 (en) 2016-06-30 2018-01-04 Janssen Pharmaceutica Nv Heteroaromatic derivatives as nik inhibitors
GB201702947D0 (en) 2017-02-23 2017-04-12 Domainex Ltd Novel compounds
CA3057891A1 (en) 2017-03-28 2018-10-04 Bayer Aktiengesellschaft Novel ptefb inhibiting macrocyclic compounds
US11254690B2 (en) 2017-03-28 2022-02-22 Bayer Pharma Aktiengesellschaft PTEFb inhibiting macrocyclic compounds
CN111247135A (zh) * 2017-10-17 2020-06-05 默克专利股份公司 嘧啶ΤΒΚ/ΙΚΚε抑制剂化合物及其用途
EP3697773A1 (en) 2017-10-17 2020-08-26 Merck Patent GmbH PYRIMIDINE TBK/IKKe INHIBITOR COMPOUNDS AND USES THEREOF
CN111727183B (zh) 2018-02-13 2023-12-29 拜耳公司 5-氟-4-(4-氟-2-甲氧基苯基)-n-{4-[(s-甲基磺亚胺酰基)甲基]吡啶-2-基}吡啶-2-胺用于治疗弥漫性大b细胞淋巴瘤中的用途
WO2020206588A1 (en) * 2019-04-08 2020-10-15 Lynk Pharmaceuticals Co., Ltd. Benzethers and anilines of pyrazolyl-amino-pyrimidinyl derivatives, and compositions and methods thereof
CN115677663A (zh) * 2022-10-25 2023-02-03 上海朴颐化学科技有限公司 一种拉米地坦中间体的制备方法

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WO2005012262A1 (en) * 2003-07-30 2005-02-10 Cyclacel Limited 2-aminophenyl-4-phenylpyrimidines as kinase inhibitors
WO2012010826A1 (en) * 2010-07-19 2012-01-26 Domainex Limited Pyrimidine compounds as inhibitors of protein kinases ikk epsilon and/or tbk-1, processes for their preparation, and pharmaceutical compositions containing them
WO2012062704A1 (en) * 2010-11-09 2012-05-18 Cellzome Limited Pyridine compounds and aza analogues thereof as tyk2 inhibitors

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GB0317841D0 (en) * 2003-07-30 2003-09-03 Cyclacel Ltd Compound
FR2911139A1 (fr) * 2007-01-05 2008-07-11 Sanofi Aventis Sa Nouveaux derives de phenyl-(4-phenyl-pyrimidin-2-yl)amines, leur preparation a titre de medicaments, compositions pharmaceutiques et notamment comme inhibiteurs de ikk
CA2698511C (en) * 2007-09-04 2016-10-11 The Scripps Research Institute Substituted pyrimidinyl-amines as protein kinase inhibitors
WO2009122180A1 (en) * 2008-04-02 2009-10-08 Medical Research Council Pyrimidine derivatives capable of inhibiting one or more kinases
NZ599826A (en) * 2009-10-12 2014-08-29 Myrexis Inc Amino-pyrimidine compounds as inhibitors of ikk epsilon and/or tbk1

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005012262A1 (en) * 2003-07-30 2005-02-10 Cyclacel Limited 2-aminophenyl-4-phenylpyrimidines as kinase inhibitors
WO2012010826A1 (en) * 2010-07-19 2012-01-26 Domainex Limited Pyrimidine compounds as inhibitors of protein kinases ikk epsilon and/or tbk-1, processes for their preparation, and pharmaceutical compositions containing them
WO2012062704A1 (en) * 2010-11-09 2012-05-18 Cellzome Limited Pyridine compounds and aza analogues thereof as tyk2 inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of WO2012142329A1 *

Also Published As

Publication number Publication date
KR20140048873A (ko) 2014-04-24
CA2832919A1 (en) 2012-10-18
JP2014510794A (ja) 2014-05-01
EP2696683A1 (en) 2014-02-19
WO2012142329A1 (en) 2012-10-18
US20140288044A1 (en) 2014-09-25
AU2012242777A1 (en) 2013-10-31
BR112013026202A2 (pt) 2017-07-25
MX2013011908A (es) 2014-03-27
CN103732067A (zh) 2014-04-16

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